1. Field of the Invention
The present invention is directed to a formulation specifically intended to induce a deep state of relaxation in a person consuming the same. An edible and appetizing delivery system may be provided, wherein the delivery system itself comprises additional and beneficial synergistic effects on the metabolism of the components of the relaxation formulation within the body. Further, a method of inducing a deep state of relaxation in a person is disclosed comprising at least the step of administering an amount of a relaxation formulation to the person.
2. Description of the Related Art
Serotonin is the common name for 5-hydroxytryptamine (“5-HT”), a monoamine neurotransmitter which is primarily found in the gastrointestinal tract, blood platelets, and the central nervous system of many animals, including human beings. Serotonin in the central nervous system is known to facilitate or increase communications between neurons allowing the central nervous system to function more effectively. It has been alleged that the effectiveness of the well known antidepressant Prozac® is due to an increase in the amount of serotonin in the synaptic gap which slightly separates individual nerve cells from one another, as a result of the drug. More in particular, serotonin has been shown to promote well being, calm, or relaxation in humans. Further, serotonin is believed to counter-balance the effects of dopamine and noradrenaline in the central nervous system, which are believed to promote arousal, fear, anger, and/or violent behavior, as well as other similarly undesirable emotions.
Tryptophan is an essential amino acid which is found in animal and vegetable protein based diets of many animals, once again, including human beings. Of the eight (8) essential amino acids and the fourteen (14) non-essential amino acids found in the foods of a normal diet, the amount of tryptophan present is the least of all. Despite its relative scarcity in the diet, the human body utilizes tryptophan for a variety of purposes. As one example, tryptophan is converted in the liver to form vitamin B3 in person's who are deficient in this essential compound. Furthermore, in person's who are even slightly deficient in vitamin B6, tryptophan may be metabolized into mildly toxic metabolites, such as hydroxykynurenine, xanthurenic acid and hydroxyanthranilic acid, within the body itself. As a result of these other processes which occur in the human body and compete for the limited amounts of tryptophan which a person obtains from their diet, it has been reported that the brain typically receives less than one (1) percent of the tryptophan present in a typical human diet.
The availability of tryptophan for conversion into serotonin in a person's brain is further limited by the blood brain barrier (“BBB”). While the BBB primarily serves to prevent toxins from entering the brain, it also serves to limit transport of amino acids, such as tryptophan, into the brain. Further exacerbating the problem is that tryptophan must complete with at least five (5) other amino acids for transport across the BBB into the brain, so as to be available for conversion into serotonin. It has been reported that the other competing amino acids may be present in amounts which are eight times the amount of tryptophan. It is also noteworthy that serotonin itself is not transported across the BBB, thus, the only serotonin available for use by the brain must be produced internally or converted from tryptophan, or its intermediate, which have crossed the BBB.
One approach which has been put forth to increase the amount of tryptophan available for transport across the BBB and conversion into serotonin in the brain is simply to provide a person with a high protein diet, thereby increasing the total amount of tryptophan ingested by the person. Unfortunately, this approach also results in proportionally increasing the amounts of other essential and non-essential amino acids which are present in the food source in the person's body. As noted above, tryptophan is the least concentrated amino acid found in most food products, and further, the tryptophan present in the food source must compete with many other amino acids present in the food for transport across the BBB. Thus, simply increasing a person's intake of tryptophan via food sources also results in an increase in other amino acids in the person's body which compete for transport across the BBB. As such, this approach, at best, only minimally increases the amount of tryptophan which ultimately crosses the BBB for conversion into serotonin.
An alternative dietary strategy is to provide a person with a high carbohydrate diet, which results in the body producing increased amounts of insulin to metabolize the additional carbohydrates to prevent elevated blood sugar levels. It has been noted that the insulin has the further effect of clearing a significant amount of amino acids present in the food source from the person's blood stream, thereby significantly minimizing the competition for the transport of tryptophan across the BBB for ultimate conversion into serotonin. Of course, this approach has a significant drawback in that the metabolism of the carbohydrates and competing amino acids from the person's blood stream by the insulin is ultimately stored as body fat.
Yet another alternative approach for increasing the availability of tryptophan for conversion into serotonin in the brain is simply to provide a person with a supplement of essentially pure tryptophan, thereby eliminating the problem of corresponding increases in the concentration of competing amino acids which are present in the person's diet. It has been shown, however, that elevated levels of tryptophan in a person's blood stream can elevate the production of an enzyme known as tryptophan pyrolase (“TP”) in the liver, which breaks down tryptophan in the body before it is able to cross the BBB. TP production is also known to be activated by the hormone cortisol which is produced in the adrenal glands when a person is under stress. Thus, a person under stress attempting to achieve a state of relaxation by taking a tryptophan supplement is actually at risk of elevated production of TP in the liver, which subsequently metabolizes the tryptophan in the blood stream before it reaches the brain for the production of serotonin. Vitamin B3 is known to inhibit TP production in the liver. Furthermore, vitamin B3 is known to activate the enzyme that converts tryptophan to 5-hydroxy-tryptophan (“5-HTP”), which is a precursor or intermediate between tryptophan and serotonin. In addition, vitamin B6 is known to activate the carboxylase enzyme which then converts 5-HTP to serotonin.
Just as tryptophan is a precursor for serotonin production, tyrosine is a precursor to the production of both dopamine and noradrenaline. The enzyme that converts tyrosine to dopamine or noradrenaline is tyrosine hydroxylase which has been found to be at least twenty-five (25) percent unsaturated in many persons. Thus, supplemental dosages of tyrosine may result in increased levels of dopamine and/or noradrenaline in a person's bloodstream, which may trigger the body to produce greater amounts of serotonin as a balance.
Melatonin is another naturally occurring compound found in many plants and animals. In particular, in human beings, melatonin is secreted into the blood by the pineal gland of the brain. More in particular, the pineal gland converts serotonin into melatonin. Melatonin supplements have been available as a sleep aid and for the treatment of certain types of insomnia. Melatonin is also believed to reduce the levels of cortisol in a person's bloodstream, and as noted above, cortisol is known to activate the liver's production of TP, an enzyme which degrades tryptophan before it is able to cross the BBB for conversion into serotonin.
Gamma-aminobutyric acid (“GABA”) is the main inhibitory neurotransmitter in the central nervous system of human beings. GABA reportedly helps reduce mental and physical stress when a person is in an over-excited state. Foods high in glutamine or theanine are believed to enhance the production of GABA in the brain. Research has shown that chocolate enhanced with GABA produced physiological stress-reducing effects, increased relaxation and immunity, while reducing anxiety in test subjects.
Therefore, it would be beneficial to provide a relaxation formulation which maximizes the amount of tryptophan available for transport across the BBB for subsequent conversion into serotonin in the brain. It would be desirable for such a relaxation formulation to incorporate components which further facilitate the conversion of tryptophan to 5-HTP and subsequent conversion to serotonin within a person's brain. It would be further helpful to provide a relaxation formulation incorporating components which inhibit metabolism of tryptophan in the person's body before it crosses the BBB, for example, inhibiting the conversion of tryptophan by TP in the liver. Another benefit may be realized by incorporating a physiologically effective amount of gamma-aminobutyric acid (“GABA”) into a relaxation formula to enhance the relaxing and stress reducing effects of the formulation experienced by a user. It would also be preferable to provide a relaxation formulation comprised solely from components which are deemed GRAS, i.e., generally recognized as safe, by the Food and Drug Administration (“FDA”), so as to minimize or eliminate FDA regulation of the same.
A further benefit would be realized by providing a delivery system for such a formulation which serves to reduce competing amino acids in a person's bloodstream so as to further facilitate the transport of tryptophan across the BBB into the person's brain for conversion into serotonin. It would also be helpful to provide a delivery system which in and of itself serves to synergistically enhance the beneficial effects of the tryptophan present in a relaxation formulation. Yet a further benefit may be realized by providing a relaxation formulation which may be vaporized for inhalation by a person in order to enhance and expedite the onset of a deep state of relaxation resulting therefrom.